pharmacology acute coronary syndrome antiplatelet and fibrinolytics

which of the following is a few antiplatelet agents

aspirin

adenosine receptor inhibitors

glycoprotein IIb/IIIa receptor inhibitors

t/f you need a balance of blood loss (hemophillia) and thrombosis

t

what is the term for blood clot formation in blood vessels?

thrombosis

what is the term for degrading of fibrin?

fibrinolytic

what is the term of inhibiting platelet activation or aggregation

antiplatelet

which of the following is a venous thrombosis?

deep vein thrombosis

pulmonary embolism

which of the following is an arterial thrombosis?

heart attack and stroke

Atherosclerosis

what clot has lots of fibrin?

red clot

what clot is rich in platelets?

white clot

in the mechanism of coagulation, what hemestasis phase causes the endothelial cells contract and release endothelins, which stimulate smooth contraction and endothelial division?

vascular phase

in the mechanism of coagulation, what hemestasis phase causes the **attachment of platelets** to sticky endothelial surfaces and as they become **activated**, platelets release a variety of chemicals that promote **aggregation**?

platelet phase

hemostasis

the stopping of the flow of blood

in the mechanism of coagulation, what hemostasis phase causes the conversion of fibrinogen into fibrin which causes a fibrin network, platelets and blood cells to be trapped in a fibrous tangle causing a blood clot?

coagulation phase

describe the coagulation phase common pathway?

activates ==factor X== → prothrombin activator → turn ==prothrombin== into thrombin → turns fibrinogen to fibrin →forms a blood clot

zymogen - something he said in class

inactive substance that is converted into an enzyme

during thrombus formation, what is secreted?

ADP, TXA2, 5-HT

what is the glycoprotein GIa?

collegen

what is glycoprotein Ib for?

von willebrand factor

what is the glycoprotein (integrin) IIb/IIIa for?

fibrinogen, macromolecule

name different types of antithrombotics?

anticoagulants: heparin,warfarin

fibrinolytics

antiplatelets

during the fibrinolytic system, what is activated to cause plasminogen to plasmin?

t-PA, urokinase

streptokinase

during the fibrinolytic system, what is inhibited

aminocaproic acid

Fibrinolysis is the process of fibrin digestion by the fibrin-specific protease. What is another word for fibrin-specific protease?

plasmin

what is present in plasma in inactive form?

plasminogen (serine protease)

fibrinolysis process (i dont understant)

plasminogen turn into plasmin ==(a2-antiplasmin)== by ==t-PA (plasminogen activator inhibitor)==→ proteolytic digestion of fibrin → thrombus remodeling

what is disseminated intravascular coagulation (DIC)?

coagulation and fibrinolytic system are pathologically activated

what does disseminated intravascular coagulation (DIC) cause?

massive tissue injury, advanced cancers, obstetric emergencies such as abruptio placentae or bacterial sepsis

what drug class is needed for thrombotic disease?

increase fibrinolysis

which of the following is a list of fibrinolytic drugs?

t-PA (recombinant alteplase)

urokinase

streptokinase

what fibrinolytic drugs are rarely used?

urokinase and streptokinase

what inhibits fibrinolysis?

aminocaproic acid

what drug is a recombinant t-PA?

==alteplase==

reteplase

tenecteplase

what drug is a ==serine protease?==

alteplase

which of the following is true about alteplase?

poor activity on plasminogen not bound to fibrin

high activity (specificity) to fibrin-bound plasminogen

what route of administration is alteplase

IV route

how is alteplase metabolized

in the liver

what is true about alteplase’s half life?

short life - 5 min

what does alteplase treat?

acute myocardial infarction, acute ischemic stroke and life threatening pulmonary embolism, DVT, thrombophlebitis with edema,

what drugs are slightly modified proteins and have longer half lives alteplase?

reteplase and tenecteplase

when should you give alteplase for acute ischemic stroke (acute MI)

within 3 hours of symptom onset

what drug reduces mortality

alteplase

whats an adverse effect of alteplase?

hemorrhage (increased bleedingrisk)

what is the moa of alteplase?

1. degradation of fibrin in hemostatic plugs at sites of vascular injury
2. 2. the systemic lytic state due to systemic generation of plasmin

what contraindication would occue with alteplase and heparin?

seruoud hemorrhage

what are some alternatives to alteplase?

mechanical reperfusion,mechanical thrombus extraction

who should not use alteplase

any bleeding liability such as peptic ulcer, intracranial hemorrhage, wounds, pregnancy, history of a cerebrovascular accident or metastatic cancer

what are some adverse effects of alteplase

bleeding, orolingual angioedema, cholesterol embolization

name some antiplatelet agents classes

prostaglandin synthesis inhibitor

adenosine receptor inhibitors

glycoprotein receptro inhibitors

misc

which of the following is a prostaglandin synthesis inhibitor?

aspirin

which of the following is adenosine receptor inhibitors

ticlopidine

clopidogrel

prasugrel

ticagrelor

cangrelor

which of the following is glycoprotein receptor inhibitors

abciximab

eptifibatide

tirofiban

what are some miscellaneous antiplatelet drugs?

dipyridamole

cilostazol

what does thromboxane A2 do?

a labile inducer of platelet aggregation and a potent vasocontrstictor

what does aspirin inhibit?

COX-1

what inhibition is ==irreversible== and acetylates a serine residue near the active site of platelet ==COX-1==?

aspirin

what is aspirin site of action/what does aspirin prevent the production of?

TXA2

what is baby aspirin - enteric coated 81 mg/day need for

dose mainly for COX-1 inhibition and affecting platelet activity

if the aspirin’s does is 325-650 mg 4-6hr, what is this for

its an analgesic/antipyretic

what drug binds to albumin

aspirin

in asprin, salicyluric acid ether or phenolic **glucuronide,** ester or acyl **glucuronide** all undergo

==liver metabolism==

what are all the effects of aspirin

inhibits arachidonic acid

inhibits COX-1

inhibits thromboxane synthase / TXA2

inhibit platelet aggregation

vasodilator

which of the ffollowing are side effects of aspirin

prolongation of bleeding, and anemia

who should not take aspirin?

patients with bleeding disorders, hypersensitivity to aspirn, and pregnant

why is aspirin not for children and infants?

reye’s syndrome

which of the following is true about aspirin

its action lasts for the lifetime of the platelet (7-10days)

which of the following drugs is high plasma protein binding?

aspirin

what is the drug interaction between NSAID and antagonize probenecid?

decreased effect

what is the drug interaction between aspirin and

methotrexate

valproic acid

NSAI

anticoagulant

sulfonylurea hypoglycemic

digoxin

increase effect

which of the following P2Y12 (ADP) receptor antagonists are irreversible blockers and prodrugs? Also standard therapy for coronary stent

ticlopidine, clopidogrel, prasugrel

which of the following are active drugs and are reversible blocker?

ticagrelor and cangrelor

which of the following is the moa of clopidogrel

it ==**irreversibly** inhibits this process==

the P2Y12 receptor couples to Gi and when activates by ADP, inhibits adenylyl cyclase, resulting in lower levels of intracellular cyclic AMP and thereby - platelet activation

which of the following is the reason why clopidogrel replaced ticlopidine?

its more potent and less toxic

what enzyme does clopidogrel reduce?

CYP2C19

what is the inactive metabolite of clopidogrel?

2-oxo-clopidogrel

what is the active metbolite of clopidogrel?

clopi-H4

what drug is commonly used with baby asprin?

clopidogrel

what is a rare interaction of clopidogrel?

thrombotic thrombocytopenic purpura

what is the drug interaction of clopidogrel and omeprazole?

inhibit CYP2C19, decrease activation of clopidogrel

what is the drug interaction between clopidogrel and opiods?

decrease absorption of clopidogrel

wjat is the drug interaction between (NSAID, warfarin, SSRI )

and clopidogrel

increase bleeding risk

what metabolizes prasugrel to thiolactone?

esterase

what metabolizes thiolactone to an active metbolite?

CYP3A4 and cyp2b6

What has no DDI with proton prump inhibitors?

prasugrel

why is clopidogrel still better than prasugrel?

prasugrel efficacy is higher but its toxicities (bleeding) is also higher than clopidogrel

which of the following is true about prasugrel?

faster onset of action

what is the drug interaction between prasugrel and these drugs: CYP3A4 inhibitors (Statins, grapefruit) and CYP3A4 inducer (rifampin)

increase bleeding

what cyp enzymes are metabolizes prasugrel?

CYP3A4, CYP2B6

which of the following is true about ticlopidine when compared to clopidogrel?

it has more adverse effects than clopidogrel

what drug is in combination with aspirin for prevention of cornary stent thrombosis?

ticlopidine

what are some adverse effects of ticlopidine?

hemorrhage

leukopenia

thrombotic thrombocytopenia purpura

which of the following drugs is a ==noncompetitive, allosteric== inhibitor of platelet activation and aggregation mediated by the P2Y12 ADP receptor?

ticagrelor

which of the following is true about ticagrelor compared to clopidogrel?

it has a rapid onset and ==**offset**== of action than clopidogrel

it has a greater and more predictable inhibition of ADP induced platelet aggregation than clopidogrel

what enzyme forma a major active metabolite for ticagrelor?

cyp3a4

how is ticagrelor excreted?

biliary secretion

what is an adverse effect of ticagrelor

dyspnea

what is the drug interaction between strong CYP3A inducer and ticagrelor

decrease efficacy

what is the drug interaction between ticagrelor and statins?

statin concetration increase

what is drug interaction between digoxin and ticagrelor?

ticagrelor weak inhibitor of p-gp. Increase digoxin level and toxicity

what ADP inhbitor drug is administered through IV?

cangrelor

what is an adverse effect of cangrelor?

bleeding is greater than with clopidogrel